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马来酸依那普利(MK-421)给药后大鼠和犬血清血管紧张素转换酶总活性

Total serum angiotensin converting enzyme activity in rats and dogs after enalapril maleate (MK-421).

作者信息

Ulm E H, Vassil T C

出版信息

Life Sci. 1982 Apr 5;30(14):1225-30. doi: 10.1016/0024-3205(82)90667-1.

Abstract

A centrifugal gel filtration separation of serum angiotensin converting enzyme (ACE) from a potent stable inhibitor is described. This, together with a 20 hr assay incubation of very dilute enzyme, permitted the assessment of the effects of enalapril maleate treatment on total serum ACE in rats and dogs. Total serum ACE increased in both species after 1 or 2 weeks at 10 mg/kg/day. Serum ACE in rats was more than doubled; whereas the increase was modest in dogs (48 +/- 9% minimum). The effect of the drug on serum ACE combined with inherent variability of ACE precluded use of serum ACE activity as an accurate measure of inhibitor concentration in animals receiving enalapril maleate.

摘要

本文描述了一种从一种强效稳定抑制剂中离心分离血清血管紧张素转换酶(ACE)的方法。这一方法,再加上对极稀酶进行20小时的测定孵育,使得能够评估马来酸依那普利治疗对大鼠和犬血清总ACE的影响。在以10mg/kg/天的剂量给药1或2周后,两种动物的血清总ACE均升高。大鼠血清ACE增加了一倍多;而犬的增加幅度较小(最低为48±9%)。该药物对血清ACE的作用以及ACE固有的变异性使得在接受马来酸依那普利的动物中,无法将血清ACE活性作为抑制剂浓度的准确测量指标。

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